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Encompassing Amino Acids: 2-500(end)
Application: Useful for the study of enzyme kinetics, screening inhibitors, and selectivity profiling.
Assay Conditions: Assay was done according to Chemi-Verse™ PKMYT1 Kinase Assay Kit (BPS Bioscience #82595) with various amounts of PKMYT1, GST-Tag Recombinant.
Background: PKMYT1 (membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase), also known as MYT1, belongs to the Wee1 serine -threonine kinase family of proteins. It inhibits CDK (cyclin dependent kinase) by phosphorylating tyrosine residues present in the ATP binding site and regulates mitosis. PKMYT1 is regulated by PKB (protein kinase B), PLK (polo-line kinase) and by CDK1. One of the most common mutations found in epithelial ovarian cancer is CCNE1 (cyclin E1) amplification, and it is a high oncogenic driver and as a predictive marker of cytotoxic chemotherapy resistance. Interestingly, the increase in CCNE1 links to a vulnerability to PKMYT1 inhibition. RP-6306 is a selective inhibitor that results in durable tumor regression in models in CCNE1 amplification. Further studies into the inhibition of PKMYT1 will uncover the potential of this protein in cancer treatment.
Description: Recombinant human full length PKMYT1 (membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase), amino acids 2-500(end). This construct contains a N-terminal GST-tag, followed by a thrombin cleavage site. This protein was affinity purified.
Format: Aqueous buffer solution
Formulation: 40 mM Tris-HCl, pH 8.0, 110 mM NaCl, 2.2 mM KCl, 0.04% Tween-20, 20% glycerol, and 3 mM MgCl2
Genbank: NM_004203
Host Cell Line: Sf9 cells
Purity: ≥85%
Tags: N-terminal GST-tag
Uniprot: Q99640
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
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